title: Efficacy of the acyclic nucleoside phosphonates (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine (FPMPA) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against feline immunodeficiency virus.
abstract: The acyclic nucleoside phosphonates (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine (FPMPA) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) were evaluated for their efficacy and side effects in a double-blind placebo-controlled trial using naturally occurring feline immunodeficiency virus (FIV)-infected cats. This natural retrovirus animal model is considered highly relevant for the pathogenesis and chemotherapy of HIV in humans. Both PMEA and FPMPA proved effective in ameliorating the clinical symptoms of FIV-infected cats, as measured by several clinical parameters including the incidence and severity of stomatitis, Karnofsky's score, immunologic parameters such as relative and absolute CD4+ lymphocyte counts, and virologic parameters including proviral DNA levels in peripheral blood mononuclear cells (PBMC) of drug-treated animals. In contrast with PMEA, FPMPA showed no hematologic side effects at a dose that was 2.5-fold higher than PMEA.
authors.affiliation: I. Medizinische Tierklinik, Ludwig-Maximilians-Universität München, Munich, Germany.
authors.forename: K
authors.initials: K
authors.lastname: Hartmann
authors.forename: M
authors.initials: M
authors.lastname: Kuffer
authors.forename: J
authors.initials: J
authors.lastname: Balzarini
authors.forename: L
authors.initials: L
authors.lastname: Naesens
authors.forename: M
authors.initials: M
authors.lastname: Goldberg
authors.forename: V
authors.initials: V
authors.lastname: Erfle
authors.forename: F D
authors.initials: FD
authors.lastname: Goebel
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
authors.forename: J
authors.initials: J
authors.lastname: Jindrich
authors.forename: A
authors.initials: A
authors.lastname: Holy
authors.forename: N
authors.initials: N
authors.lastname: Bischofberger
authors.forename: W
authors.initials: W
authors.lastname: Kraft
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D000998:Antiviral Agents / Q000627:therapeutic use*; D018791:CD4 Lymphocyte Count / Q000187:drug effects; D002415:Cats; D004311:Double-Blind Method; D016181:Feline Acquired Immunodeficiency Syndrome / Q000097:blood / Q000188:drug therapy*; D005260:Female; D017567:Karnofsky Performance Status; D008297:Male; D063065:Organophosphonates / Q000493:pharmacokinetics / Q000627:therapeutic use* / Q000633:toxicity; D010919:Placebos; D012015:Reference Standards; D013280:Stomatitis / Q000188:drug therapy / Q000662:veterinary; D019562:Viral Load
chemical_list: D000998:Antiviral Agents; D063065:Organophosphonates; D010919:Placebos; C069328:9-(3-fluoro-2-phosphonylmethoxypropyl)adenine; C053001:adefovir; D000225:Adenine